Lipid Lowering Drugs (Antilipemic Drugs) (53)

Question 1

What are the two primary forms of lipids in the blood

Answer 1

Triglycerides and cholesterol

Question 2

Triglycerides and cholesterol are __ soluble __’s that must be packaged for transport in blood

Answer 2

Water soluble fats

Question 3

____ are the combination of lipids with protein

Answer 3

Lipoproteins

Question 4

Lipoproteins

Answer 4

Lipids + proteins

Question 5

lipids

Answer 5

Cholesterol, TGs, others

Question 6

Proteins

Answer 6

On the surface of the particle

Question 7

Chylomicrons are from

Answer 7

The GI tract

Question 8

Very low density lipoprotein

Answer 8

Produced by liver and transports TGs to cells

Question 9

Low density lipoprotein

Answer 9

Less desired, bad cholesterol
-cholesterol rich
-cell membranes and steroid hormones

Question 10

High density lipoprotein

Answer 10

Highly desired
-responsible for recycling of cholesterol
-also known as good cholesterol

Question 11

Non modifiable factors of coronary artery disease

Answer 11

Age, family history, strong history of premature CAD

Question 12

Age risk factors of CAD: male/female

Answer 12

Male- 45+

Female- 55+

Question 13

Modifiable factors of CAD

Answer 13

-current cigarette smoker
-abdominal obesity
-hypertension
-DM
-LDL:HDL ratio

Question 14

Four groups of lipid lowering drugs

Answer 14

-HMG CoA reductase inhibitors
-inhibitors of cholesterol absorption
-niacin
-fibric acid derivatives

Question 15

HMG-CoA

Answer 15

3-hydroxy-3-methylglutaryl coenzyme A
-one of metabolites in cholesterol synthesis pathway

Question 16

HMG-CoA reductase

Answer 16

Critical enzyme for liver cholesterol production

Question 17

HMG-CoA reductase inhibitors reduce..

Answer 17

Plasma LDL levels

Question 18

Example of HMG-CoA reductase inhibtors

Answer 18

Atorvastatin
-end in statin!!!

Question 19

HMG-CoA reductase inhibtors MOA

Answer 19

Inhibit HMG-CoA reductase
-which is an important liver enzyme that produces cholesterol

Question 20

HMG-CoA reductase inhibtors lower the rate of

Answer 20

Cholesterol production
-inc liver LDL receptors
-inc plasma clearance of LDL

Question 21

Added benefits of statins

Answer 21

-decrease VLDL (carry TGs)
-raise HDL (improve LDL/HDL)

Question 22

HMG-CoA reductase inhibtors indications

Answer 22

-first line drug therapy for hyper cholesterol Emma
-treatment of types IIa and IIb hyperlipidemias (high LDL) levels

Question 23

HMG-CoA reductase inhibtors adverse effects

Answer 23

-GI disturbances
-headache
-muscle pain (myalgia)
-liver injury (raised enzymes)

Question 24

Contraindications of HMG-CoA reductase inhibtors

Answer 24

Not used during pregnancy

Question 25

Grapefruit and grapefruit juice

Answer 25

Inhibit CYP3A4

Question 26

Three examples of drug inhibitors of CYP3A4

Answer 26

-warfarin -erythromycin -ritonavir

Question 27

(2) drugs that inhibit cholesterol absorption

Answer 27

-bile acid binding resins -ezetimibe

Question 28

(2) examples of bile acid binding resins

Answer 28

Cholestyramine, colestipol

Question 29

When are Cholestyramine, Colestipol taken?

Answer 29

Taken before meals (Bile acid binding resins)

Question 30

Ezetimibe

Answer 30

Inhibits cholesterol absorption

Question 31

MOA of bile acid sequestration

Answer 31

Prevent reabsorption of bile acids from small intestine

Question 32

Where are bile acids synthesized

Answer 32

Synthesized from cholesterol in liver

Question 33

What is the liver stimulated to do?

Answer 33

Produce more bile acids

Question 34

Indications of bile acid sequestrants

Answer 34

-type II hyperlipoproteinemia -relief of pruritus associated with partial biliary obstruction

Question 35

Cholestyramine specific Indications

Answer 35

Relief of pruritus

Question 36

AE of bile acid sequestrants

Answer 36

-GI (constipation, heartburn, nausea, belching, bloating) -decrease absorption of fat soluble vitamins (A,D,E,K)

Question 37

Examples of fat soluble vitamins (4)

Answer 37

A, D, E, K

Question 38

AE of bile acid sequestrants tend to what..

Answer 38

Disappear over time

Question 39

fibric acid derivatives MOA (2)

Answer 39

Believed* -activate lipoproteins lipase -breaks down TGs in lipoproteins -reduce plasma TGs Also -inc fatty acid use in tissues

Question 40

fibric acid derivatives decrease….

Answer 40

Plasma triglyceride levels

Question 41

fibric acid derivatives increase…

Answer 41

HDL by as much as 10-25%

Question 42

(3) examples of fibric acid derivatives

Answer 42

-gemfibrozil -bezafibrate -fenofibrate

Question 43

fibric acid derivatives AE

Answer 43

-GI (discomfort, diarrhea, nausea) -blurred vision -risk of gallstones -prolonged prothrombin time

Question 44

AE fibric acid derivatives: prolonged prothrombin time

Answer 44

-fibrinogen production is reduced -displacement of anticoagulants from albumin

Question 45

Nicotinic acid or Niacin =

Answer 45

Vitamin B3

Question 46

Niacin MOA

Answer 46

Reduces plasma TGs

Question 47

Niacin properties

Answer 47

-lipid lowering properties

Question 48

Niacin as a vitamin

Answer 48

Requires much higher doses (grams) for lipid lowering properties

Question 49

Pro: Niacin

Answer 49

Effective, inexpensive, often used in combination with other lipid lowering agents (statins)

Question 50

MOA nicotinic acid

Answer 50

Reduces VLDL (carries TGs) from liver -inhibit lipase = breakdown of lipids -less fatty acid for TG production in liver

Question 51

AE nicotinic acid

Answer 51

-flushing -pruritus -GI distress

Question 52

Why does Nicotinic Acid cause flushing, and can it be prevented

Answer 52

Due to PG release -prevent by taking aspirin 30 min before